Date published: 2026-5-16

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α2-Macroglobulin Inhibitors

Chemical inhibitors of α2-Macroglobulin offer various mechanisms by which they can impede the protein's protease-binding function. E-64 is one such chemical that forms a covalent adduct with the active cysteine residue in the protease domain of α2-Macroglobulin, thereby causing an irreversible inhibition. Similarly, Estatin interacts with cysteine residues at the active site, obstructing the protease-binding ability of the protein. Phosphoramidon takes a different approach by targeting the metalloprotease active site, crucial for the interaction between proteases and α2-Macroglobulin, and blocks it to prevent binding. Marimastat and Ilomastat also inhibit the interaction with metalloproteases by binding to the protein's metalloprotease domain; however, they do so by interacting with the catalytic domain of matrix metalloproteases that are targets of α2-Macroglobulin.

On the other hand, Pepstatin A inhibits α2-Macroglobulin by binding to aspartic residues within the protease's active site, which are essential for the proteolytic cleavage of substrates. Leupeptin and Antipain, which are reversible inhibitors of serine and cysteine proteases, interact with the catalytic site of α2-Macroglobulin, preventing the hydrolysis of peptide bonds. Aprotinin and Gabexate mesilate, both of which are known to primarily inhibit serine proteases, bind to the active site of α2-Macroglobulin and inhibit its function. Bestatin, as an aminopeptidase inhibitor, prevents the degradation of peptide substrates by blocking access to α2-Macroglobulin's binding sites for proteolytic enzymes. Meanwhile, Chymostatin specifically binds to and blocks the chymotrypsin-like proteases that α2-Macroglobulin may target, thus inhibiting the protein's protease activity. Each chemical inhibitor utilizes a unique method to inhibit α2-Macroglobulin, resulting in the reduction of its functional proteolytic activity in various capacities.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

E-64

66701-25-5sc-201276
sc-201276A
sc-201276B
5 mg
25 mg
250 mg
$281.00
$947.00
$1574.00
14
(0)

E-64 is a potent, irreversible cysteine protease inhibitor that can inhibit the proteolytic activity of α2-Macroglobulin by forming a covalent adduct with the active cysteine residue in the protease domain of the protein.

Phosphoramidon

119942-99-3sc-201283
sc-201283A
5 mg
25 mg
$199.00
$632.00
8
(1)

Phosphoramidon is a metalloprotease inhibitor that can inhibit the protease-binding function of α2-Macroglobulin by blocking the metalloprotease active site, which is necessary for the protein's interaction with proteases.

Leupeptin hemisulfate

103476-89-7sc-295358
sc-295358A
sc-295358D
sc-295358E
sc-295358B
sc-295358C
5 mg
25 mg
50 mg
100 mg
500 mg
10 mg
$73.00
$148.00
$316.00
$499.00
$1427.00
$101.00
19
(3)

Leupeptin is a reversible inhibitor of serine and cysteine proteases that inhibits the proteolytic function of α2-Macroglobulin by interacting with its catalytic site, preventing the hydrolysis of peptide bonds in proteins.

Chymostatin

9076-44-2sc-202541
sc-202541A
sc-202541B
sc-202541C
sc-202541D
5 mg
10 mg
25 mg
50 mg
100 mg
$156.00
$260.00
$640.00
$1186.00
$2270.00
3
(1)

Chymostatin is a chymotrypsin inhibitor that can inhibit the protease activity of α2-Macroglobulin by specifically binding to and blocking the chymotrypsin-like proteases that α2-Macroglobulin may target.

Aprotinin

9087-70-1sc-3595
sc-3595A
sc-3595B
10 mg
100 mg
1 g
$112.00
$408.00
$3000.00
51
(2)

Aprotinin is a protease inhibitor that primarily inhibits serine proteases and can inhibit the protease-binding function of α2-Macroglobulin by preventing the interaction with various serine proteases.

Bestatin

58970-76-6sc-202975
10 mg
$131.00
19
(3)

Bestatin is an aminopeptidase inhibitor that prevents the degradation of peptide substrates, and it can inhibit the protease activity of α2-Macroglobulin by blocking access to the binding sites for proteolytic enzymes.

Marimastat

154039-60-8sc-202223
sc-202223A
sc-202223B
sc-202223C
sc-202223E
5 mg
10 mg
25 mg
50 mg
400 mg
$168.00
$218.00
$404.00
$629.00
$4900.00
19
(1)

Marimastat is a broad-spectrum matrix metalloprotease (MMP) inhibitor that can inhibit the protease activity of α2-Macroglobulin by binding to the protein's metalloprotease domain, preventing its interaction with various MMPs.

Gabexate mesylate

56974-61-9sc-215066
5 mg
$100.00
(0)

Gabexate mesilate is a serine protease inhibitor that can inhibit the protease activity of α2-Macroglobulin by binding to its active site, thereby obstructing the proteolytic processing of α2-Macroglobulin's target proteases.

GM 6001

142880-36-2sc-203979
sc-203979A
1 mg
5 mg
$77.00
$270.00
55
(1)

Ilomastat is a synthetic matrix metalloprotease inhibitor that can inhibit the function of α2-Macroglobulin by binding to the catalytic domain of MMPs which α2-Macroglobulin targets, thereby preventing the protease-protein complex formation.